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HUP0401538A2 - Novel derivatives of n-(arylsulfonyl)beta-aminoacids comprising a substituted aminomethyl group, the preparation method thereof and pharmaceutical compositions containing same - Google Patents

Novel derivatives of n-(arylsulfonyl)beta-aminoacids comprising a substituted aminomethyl group, the preparation method thereof and pharmaceutical compositions containing same

Info

Publication number
HUP0401538A2
HUP0401538A2 HU0401538A HUP0401538A HUP0401538A2 HU P0401538 A2 HUP0401538 A2 HU P0401538A2 HU 0401538 A HU0401538 A HU 0401538A HU P0401538 A HUP0401538 A HU P0401538A HU P0401538 A2 HUP0401538 A2 HU P0401538A2
Authority
HU
Hungary
Prior art keywords
optionally substituted
group
aminoacids
arylsulfonyl
beta
Prior art date
Application number
HU0401538A
Other languages
Hungarian (hu)
Inventor
Bernard Ferrari
Jean Gougat
Yvette Muneaux
Pierre Perreaut
Lionel Sarran
Original Assignee
Sanofi-Synthelabo
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Sanofi-Synthelabo filed Critical Sanofi-Synthelabo
Publication of HUP0401538A2 publication Critical patent/HUP0401538A2/en
Publication of HUP0401538A3 publication Critical patent/HUP0401538A3/en

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    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/36—Radicals substituted by singly-bound nitrogen atoms
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Abstract

A találmány az (I) általános képletű vegyületekre vonatkozik, aképletben R1 jelentése fenilvinilcsoport, adott esetben helyettesítettfenil-, naftil-, tetrahidronaftil- vagy heterociklusos csoport; R2jelentése hidrogénatom vagy alkilcsoport, és R3 jelentése adott esetben helyettesített fenil- vagyheterociklusos csoport; vagy R2 jelentése adott esetben helyettesítettfenil- vagy heterociklusos csoport, és R3 jelentése hidrogénatom; R4jelentése adott esetben helyettesített karbamoil- vagytiokarbamoilcsoport, fenilkarbonil-, tiazolkarbonil- vagypiridilkarbonilcsoport; R5 jelentése adott esetben helyettesítettaminometilcsoport. A vegyületek a bradikinin receptorok iránt mutatnakaffinitást és a B1 receptorok vonatkozásában szelektívek; olyangyógyszertermékek előállítására használhatók, amelyek gyulladásospatológiák és tartós vagy krónikus gyulladásos betegségek kezelésérevagy megelőzésére alkalmasak. A találmány tárgya továbbá az (I)általános képletű vegyületek előállítására vonatkozó eljárás, valamintannak intermedierjei. ÓThe invention relates to compounds of general formula (I), in which R1 is a phenylvinyl group, optionally a substituted phenyl, naphthyl, tetrahydronaphthyl or heterocyclic group; R2 is a hydrogen atom or an alkyl group, and R3 is an optionally substituted phenyl or heterocyclic group; or R 2 is an optionally substituted phenyl or heterocyclic group and R 3 is a hydrogen atom; R4 is optionally substituted carbamoyl or thiocarbamoyl, phenylcarbonyl, thiazolecarbonyl or pyridylcarbonyl; R5 is an optionally substituted aminomethyl group. The compounds show affinity for bradykinin receptors and are selective for B1 receptors; they can be used to produce pharmaceutical products that are suitable for the treatment or prevention of inflammatory pathologies and persistent or chronic inflammatory diseases. The subject of the invention is also the process for the production of compounds of general formula (I) and their intermediates. HE

HU0401538A 2001-03-28 2002-03-27 Novel derivatives of n-(arylsulfonyl)beta-aminoacids comprising a substituted aminomethyl group, the preparation method thereof and pharmaceutical compositions containing same HUP0401538A3 (en)

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FR0104315A FR2822827B1 (en) 2001-03-28 2001-03-28 NOVEL N- (ARYLSULFONYL) BETA-AMINOACIDS DERIVATIVES COMPRISING A SUBSTITUTED AMINOMETHYL GROUP, THEIR PREPARATION METHOD AND THE PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME
PCT/FR2002/001059 WO2002076964A1 (en) 2001-03-28 2002-03-27 Derivatives of n-(arylsulfonyl)beta-aminoacids comprising a substituted aminomethyl group, the preparation method thereof and the pharmaceutical compositions containing same

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NO20034267L (en) 2003-11-28
KR20030089704A (en) 2003-11-22
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BR0208489A (en) 2004-03-30
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HUP0401538A3 (en) 2008-05-28
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